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SP2509

Cat. No. M6143
SP2509 Structure
Synonym:

HCI-2509

Size Price Availability Quantity
5mg USD 95 In stock
10mg USD 145 In stock
50mg USD 450 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

In vitro: In AML cells, SP2509 inhibits the association of LSD1 with CoREST, increases promoter-specific H3K4Me3 and induces p53, p21 and C/EBPα. SP2509 also significantly inhibits the colony growth and induces apoptosis of OCI-AML3. In addition, SP2509 induces differentiation of cultured and primary AML cells, and exerts synergistic lethal activity when used in combination with panobinostat.

In vivo: In mice bearing OCI-AML3 xenografts, SP2509 (25 mg/kg i.p.) significantly improved the survival of the mice, while co-treatment with SP2509 and panobinostat exerts superior in vivo activity.

Protocol
Cell Experiment
Cell lines OCI-AML3, MV4-11 and MOLM13 cells
Preparation method Cultured AML cells are treated with SP2509 and/or PS for 96 h. At the end of treatment, cells are washed free of the drugs and 500 cells per condition are plated in methylcellulose and incubated at 37 °C. Colony formation is measured 7–10 days after plating.
Concentrations ~10 μM
Incubation time 96 h
Animal Experiment
Animal models NOD/SCID mice bearing OCI-AML3 xenografts
Formulation 20% Cremaphor, 20% DMSO, 60% sterile water
Dosages 25 mg/kg twice per week
Administration i.p.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 437.90
Formula C19H20ClN3O5S
CAS Number 1423715-09-6
Purity >99%
Solubility 38 mg/mL in DMSO
Storage at -20°C
References

Stepwise assembly of functional C-terminal REST/NRSF transcriptional repressor complexes as a drug target.
Inui K, et al. Protein Sci. 2017 May;26(5):997-1011. PMID: 28218430.

Highly effective combination of LSD1 (KDM1A) antagonist and pan-histone deacetylase inhibitor against human AML cells.
Fiskus W, et al. Leukemia. 2014 Nov;28(11):2155-64. PMID: 24699304.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SP2509, HCI-2509 supplier, Histone demethylases, inhibitors

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